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搜索结果：“azd”

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AZD1390

Catalog No. A16798
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ATM 抑制剂

AZD1390是一流的口服中枢神经渗透性ATM抑制剂，在细胞中的IC50为0.78 nM，对PIKK酶家族中密切相关的成员具有10,000倍以上的选择性，并且在多种激酶中均具有出色的选择性。了解更多

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AZD0156

Catalog No. A16419
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ATM 抑制剂

AZD0156是有效且选择性的ATM激酶抑制剂，具有潜在的化学/放射致敏和抗肿瘤活性。了解更多

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- Yi-Ru Pan, .et al. ATM Inhibitor Suppresses Gemcitabine-Resistant BTC Growth in a Polymerase θ Deficiency-Dependent Manner, Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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AZD8835

Catalog No. A16352
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PI3Kα/PI3Kδ 抑制剂

AZD8835是一种有效的选择性PI3Kα和PI3Kδ抑制剂，IC50为5.7 nM和6.2 nM，对PI3Kβ（IC50 431 nM）和PI3Kγ（IC50 90 nM）具有选择性。了解更多

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- James T. Lynch, etc. Identification of differential PI3K pathway target dependencies in T-cell acute lymphoblastic leukemia through a large cancer cell panel screen. Oncotarget. 2016 Apr 19; 7(16): 22128–22139.
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AZD3264

Catalog No. A15900
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IKK2 抑制剂?

AZD3264是一种新型的IKK2抑制剂。了解更多

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AZD9496

Catalog No. A15822
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estrogen receptor downregulator and 拮抗剂

AZD9496是一种有效的生物选择性雌激素受体下调剂和拮抗剂。了解更多

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AZD1283

Catalog No. A15443
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P2Y12 receptor 拮抗剂

AZD1283是P2Y12受体的有效拮抗剂，EC50为3.0 ug/kg/min，TI> 10；结合IC50为11 nM。了解更多

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AZD6738 (Ceralasertib)

Catalog No. A15794
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ATR 抑制剂

AZD6738是一种有效的ATR激酶抑制剂，对分离的酶的IC50为1 nM，对细胞中ATR激酶依赖性CHK1磷酸化的IC50为74 nM。了解更多

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- Brian F Kiesel, .et al. Dose-dependent bioavailability and tissue distribution of the ATR inhibitor AZD6738 (ceralasertib) in mice, Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. The POLD1 R689W variant increases the sensitivity of colorectal cancer cells to ATR and CHK1 inhibitors, Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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AZD8186

Catalog No. A15759
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PI3K 抑制剂

AZD8186是一种同工型特异性小分子PI3K抑制剂，有效抑制PI3Kβ（IC50 = 4 nM）和PI3Kδ（IC50 = 12 nM），选择性高于PI3Kα（IC50 = 35 nM）和PI3Kγ（IC50 = 675 nM）。了解更多

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AZD7687

Catalog No. A15012
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DGAT1 抑制剂

AZD7687是一种有效的选择性DGAT1抑制剂，IC50值为80 nM（hDGAT1）。了解更多

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AZD1152

Catalog No. A15011
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Aurora B 抑制剂

AZD1152是一种前药，可在血清中迅速经历磷酸酶介导的裂解作用，释放出Barasertib-hQPA（一种选择性的Aurora B激酶抑制剂），在急性髓细胞性白血病（AML）患者的临床研究中显示出初步活性。了解更多

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AZD4017

Catalog No. A13542
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HSD1 抑制剂

AZD4017是一种有效的，选择性的，口服可生物利用的11b-HSD1抑制剂（11b-羟基类固醇脱氢酶1型抑制剂）。了解更多

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AZD8186

Catalog No. A14164
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PI3K 抑制剂

AZD8186是磷酸肌醇-3激酶(PI3K)β亚型的抑制剂，具有潜在的抗肿瘤活性。了解更多

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AZD6642

Catalog No. A14400
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FLAP 抑制剂

AZD6642是5-Lipoxygenase激活蛋白（FLAP）的抑制剂，可用于治疗炎症。了解更多

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Alvelestat

Catalog No. A12779
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neutrophil elastase 抑制剂

Avelestat，也称为AZD9668，是可口服的,高度选择性neutrophil elastase (NE)抑制剂，IC50和Ki分别为12 nM和9.4 nM,其选择性超过其他丝氨酸蛋白酶至少600倍。了解更多

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AZD1981

Catalog No. A13186
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CRTH2 receptor 拮抗剂

AZD1981作为疾病相关细胞系统的有效拮抗剂，可抑制DK-PGD2诱导的人嗜酸性粒细胞CD11b表达，IC50为10 nM。了解更多

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AZD3463

Catalog No. A13065
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ALK/IGF1R 抑制剂

AZD3463是ALK/IGF1R抑制剂。了解更多

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AZD5423

Catalog No. A13249
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nonsteroidal glucocorticoid receptor 激动剂

AZD5423是新型的非甾体类糖皮质激素受体激动剂。了解更多

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AZD2858

Catalog No. A13060
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GSK-3β 抑制剂

AZD2858是一种选择性GSK-3抑制剂，IC50为68 nM，激活Wnt信号，增加大鼠的骨量。了解更多

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AZD1208

Catalog No. A13203
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pan-Pim kinase 抑制剂

AZD1208是PIM激酶的小分子抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Remy J, .et al. Inhibition of PIM1 blocks the autophagic flux to sensitize glioblastoma cells to ABT-737-induced apoptosis, Biochim Biophys Acta Mol Cell Res, 2019, Feb;1866(2):175-189 PMID: 30389373
- Andrea L. Casillas, .et al. Hypoxia-inducible PIM kinase expression promotes resistance to anti-angiogenic agents, Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
- Sathish K.R. Padi, .et al. Targeting the PIM protein kinases for the treatment of a T-cell acute lymphoblastic leukemia subset, Oncotarget, 2017, May 2; 8(18): 30199-30216 PMID: 28415816
- Lim R, .et al. Inhibition of PIM1 kinase attenuates inflammation-induced pro-labour mediators in human foetal membranes in vitro, Mol Hum Reprod, 2017, Jun 1;23(6):428-440 PMID: 28333279
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AZD3514

Catalog No. A12396
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AR 抑制剂 downregulator

AZD3514是一种有效的雄激素受体下调剂，具有潜在的抗癌活性。了解更多

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AZD1080

Catalog No. A12819
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GSK3 抑制剂

AZD1080是一种新型GSK3抑制剂，可消除啮齿动物大脑中的突触可塑性缺陷，并在人类中表现出外周靶标参与。了解更多

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- Shengzhong Liu, .et al. STAT1-avtiviated LINC00961 regulates myocardial infarction by the PI3K/AKT/GSK3?? signaling pathway, J Cell Biochem, 2019, 2019
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AZD3839

Catalog No. A12825
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BACE1 抑制剂

AZD3839是人类BACE1的有效选择性抑制剂，Ki为26.1 nM。了解更多

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AZD5363

Catalog No. A11759
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AKT 抑制剂

AZD5363是有效的AKT抑制剂，在体内具有药效学活性，有潜力作为单一疗法或联合用药来治疗一系列实体瘤和血液肿瘤。了解更多

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- Giri R. Gnawali, .et al. Synthesis of 2-oxoquinoline derivatives as dual pim and mTORC protein kinase inhibitors, Medicinal Chemistry Research, 2022, 31: 1154-1175
- Jeremiah J Bearss, .et al. EDC3 phosphorylation regulates growth and invasion through controlling P-body formation and dynamics, EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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AZD3759

Catalog No. A15551
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EGFR 抑制剂

AZD3759是表皮生长因子受体（EGFR）的口服抑制剂。它结合并抑制EGFR以及某些突变形式的EGFR的活性。了解更多

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AZ5104

Catalog No. A15516
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EGFR 抑制剂

AZD-9291的去甲基代谢产物AZ5104是一种有效的EGFR抑制剂，对于EGFR（L858R/T790M），EGFR（L858R），EGFR（L861Q）和EGFR，IC50 <1 nM，6 nM，1 nM和25 nM EGFR（野生型）。了解更多

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AZD5597

Catalog No. A13506
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CDK 抑制剂

AZD5597是有效的CDK抑制剂，对一系列癌细胞具有体外抗增殖作用。了解更多

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AZD2014 (Vistusertib)

Catalog No. A11303
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mTORC1/2 抑制剂

Vistusertib (AZD2014)是一种新型mTOR抑制剂，无细胞试验中IC50为2.8 nM；对多种PI3K亚型(α/β/γ/δ)具有较高选择性。浓度为1 μM时，对大多数激酶无或有微弱结合力。了解更多

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- Shuhang Dai, .et al. Calcium/calmodulin-dependent protein kinase kinase 2 mediates pleiotropic effects of epidermal growth factor in cancer cells, Biochim Biophys Acta Mol Cell Res, 2022, Jul;1869(7):119252 PMID: 35271909
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Ticagrelor (AZD6140)

Catalog No. A11238
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P2Y12 拮抗剂

Ticagrelor (AZD6140)是第一个可逆结合的口服P2Y（12）受体拮抗剂，可阻断ADP诱导的血小板聚集。了解更多

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AZD5438

Catalog No. A11105
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CDK 抑制剂

AZD5438是有效的细胞周期蛋白依赖性激酶（CDK）1、2和9抑制剂（IC50值分别为16、6和20 nM）。了解更多

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AZD4547

Catalog No. A11075
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FGFR 抑制剂

AZD4547是一种有效，选择性和口服活性的pan-FGFR抑制剂，对于FGFR1、2、3和4的IC50分别为0.2、2.5、1.8和165 nM。了解更多

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- Ryuma Tokunaga, .et al. Fibroblast growth factor receptor 2 expression, but not its genetic amplification, is associated with tumor growth and worse survival in esophagogastric junction adenocarcinoma, Oncotarget, 2016, Apr 12; 7(15): 19748-19761 PMID: 26933914
- Mitsuko Kawano, .et al. FGF18 signaling in the hair cycle resting phase determines radioresistance of hair follicles by arresting hair cycling, Adv Radiat Oncol, 2016, Jul-Sep; 1(3): 170-181 PMID: 28740887
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AZD8330

Catalog No. A10115
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MEK 抑制剂

AZD8330是新型，选择性，非ATP竞争性MEK 1/2抑制剂，IC50为7 nM。阶段1。了解更多

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MK-1775

Catalog No. A10599
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WEE1 抑制剂

MK-1775是一种有效的体外和体内Wee1激酶抑制剂。了解更多

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- Ting-Yu Chang, .et al. A novel histone deacetylase inhibitor MPT0L184 dysregulates cell-cycle checkpoints and initiates unscheduled mitotic signaling, Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- 2018, .et al. Augmentation of the therapeutic efficacy of WEE1 kinase inhibitor AZD1775 by inhibiting the YAP-E2F1-DNA damage response pathway axis, FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Rulina AV, .et al. Distinct outcomes of CRL-Nedd8 pathway inhibition reveal cancer cell plasticity, Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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AZD7762

Catalog No. A10113
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Chk1 & Chk2 抑制剂

AZD7762是一种有效的ATP竞争性检查点激酶抑制剂，可促进检查点废止并增强DNA靶向疗法。了解更多

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AZD8931 (Sapitinib)

Catalog No. A10116
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pan-EGFR/pan-erbB 抑制剂

AZD8931 (Sapitinib)是ErbB1，ErbB2和ErbB3受体信号传导的等效抑制剂。了解更多

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- Takeshi Ito, .et al. Mathematical analysis of gefitinib resistance of lung adenocarcinoma caused by MET amplification, Biochem Biophys Res Commun, 2019, in Press
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AZD6482

Catalog No. A10112
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PI3K 抑制剂

AZD6482是一种PI3Kβ抑制剂，(IC50 = 0.021M)。了解更多

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Saracatinib (AZD0530)

Catalog No. A10108
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Src/Abl 抑制剂

Saracatinib (AZD0530)是一种高选择性，双特异性Src/Abl激酶抑制剂，对c-Src和Abl激酶的IC50分别为2.7和30 nM。了解更多

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- Andromachi Lambrianidou, .et al. mTORC2 deploys the mRNA binding protein IGF2BP1 to regulate c-MYC expression and promote cell survival, Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Chisato Naito, .et al. Facilitatory effects of fetuin-A on atherosclerosis, Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. 5-Azacytidine-induced Protein 2 (AZI2) Regulates Bone Mass by Fine-tuning Osteoclast Survival, J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. Emerging therapies: angiogenesis inhibitors for ovarian cancer, Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
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AZD8055

Catalog No. A10114
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mTOR 抑制剂

AZD8055是一种有效的，选择性的ATP竞争性mTOR激酶抑制剂，IC50为0.8 nM。了解更多

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- L. M. C. Koene, .et al. Effects of antiepileptic drugs in a new TSC/mTOR-dependent epilepsy mouse model, ACTN, 2019, June PMID: 31353861
- Helga Weber, .et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice, Oncotarget, 2015, Oct 13; 6(31): 31877–31888 PMID: 26397134
- Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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AZD6244 (Selumetinib)

Catalog No. A10257
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MEK 抑制剂

Selumetinib (AZD6244)是一种有效，高选择性的MEK抑制剂，ARRY142886，AZD-6244和ARRY-142886是MEK 1/2抑制剂，GI50值在14至50 nm之间。了解更多

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- Chia-Chi Chang, .et al. Upregulation of lactate dehydrogenase a by 14-3-3ζ leads to increased glycolysis critical for breast cancer initiation and progression, Oncotarget, 2016, Jun 7; 7(23): 35270-35283 PMID: 27150057
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AZ7550

Catalog No. A12008
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IGF1R inhibitor

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM. 了解更多

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AZD8797

Catalog No. A21230
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human CX3CR1 receptor modulator

AZD8797 is an allosteric non-competitive and orally active modulator of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively. 了解更多

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Tenapanor

Catalog No. A14011
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NHE3 抑制剂

Tenapanor充当钠-质子交换器NHE3的抑制剂。这种抗转运蛋白在肾脏和肠道中发现，通常起到调节机体吸收和分泌的钠水平的作用。了解更多

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- Xingjie Tan, .et al. The Na+/H+ exchanger NHE3 inhibitor tenapanor prevents intestinal obstructions in CFTR-deleted mice, Authorea, 2022, May 25
- Kunyan Zhou, .et al. Functional characterization of the sodium/hydrogen exchanger 8 and its role in proliferation of colonic epithelial cells, Am J Physiol Cell Physiol, 2021, Sep 1;321(3):C471-C488 PMID: 34288721
- Qinghai Tan, .et al. Inhibition of Na + /H + exchanger isoform 3 improves gut fluidity and alkalinity in cystic fibrosis transmembrane conductance regulator-deficient and F508del mutant mice, Br J Pharmacol, 2021, Mar;178(5):1018-1036 PMID: 33179259
- Y Liu, .et al. Deciphering Ion Transporters, Kinases and PDZ-adaptor Molecules That Mediate Guanylate Cyclase C Agonist-Dependent Intestinal Fluid Loss in Vivo, Biochem Pharmacol, 2020, May 16;178:114040 PMID: 32422138
- Yu Y, .et al. Expression, Localization and Functional Activity of the Major Na+/H+ Exchange Isoforms Expressed in the Intestinal Cell Line Caco-2BBe, Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thammayon N, .et al. Na+/H+ exchanger 3 inhibitor diminishes the amino-acid-enhanced transepithelial calcium transport across the rat duodenum, Amino Acids, 2017, Apr;49(4):725-734 PMID: 27981415
- Charoenphandhu N, .et al. Na+/H+ exchanger 3 inhibitor diminishes hepcidin-enhanced duodenal calcium transport in hemizygous β-globin knockout thalassemic mice, Mol Cell Biochem, 2017, Mar;427(1-2):201-208 PMID: 27995414
- Jantarajit W, .et al. CFTR-mediated anion secretion across intestinal epithelium-like Caco-2 monolayer under PTH stimulation is dependent on intermediate conductance K+ channels, Am J Physiol Cell Physiol, 2017, Jul 1;313(1):C118-C129 PMID: 28490422
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AZD1152-HQPA (Barasertib)

Catalog No. A10109
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Aurora Kinase B 抑制剂

AZD1152-HQPA (Barasertib)是Aurora B的高效抑制剂，Ki值分别为0.36（Aurora B）和1369 nM（Aurora A），与一组其他50种激酶相比具有很高的特异性。了解更多

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- Sakamoto K, .et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 PMID: 29795241
- Jennifer M. Sahni, .et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases, J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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Olaparib (AZD2281)

Catalog No. A10111
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PARP 抑制剂

Olaparib (AZD2281)是聚ADP核糖聚合酶（PARP）的抑制剂，该酶是一种与DNA修复有关的酶。了解更多

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- Saptarshi Sinha, .et al. Olaparib enhances the Resveratrol-mediated apoptosis in breast cancer cells by inhibiting the homologous recombination repair pathway, Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. Combination of talazoparib and olaparib enhanced the curcumin-mediated apoptosis in oral cancer cells by PARP-1 trapping, J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. DNA damage promotes HLA class I presentation by stimulating a pioneer round of translation-associated antigen production, Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. ARL6IP5 reduces cisplatin-resistance by suppressing DNA repair and promoting apoptosis pathways in ovarian carcinoma, Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents, Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. BRCA1/ATF1-Mediated Transactivation is Involved in Resistance to PARP Inhibitors and Cisplatin, Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. Evolutionary dynamics of cancer multidrug resistance in response to olaparib and photodynamic therapy, Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity, Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. Olaparib enhances curcumin-mediated apoptosis in oral cancer cells by inducing PARP trapping through modulation of BER and chromatin assembly, DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. Persistence of RNA transcription during DNA replication delays duplication of transcription start sites until G2/M, Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. Metolazone upregulates mitochondrial chaperones and extends lifespan in Caenorhabditis elegans, Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement, Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
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Cediranib (AZD2171)

Catalog No. A10185
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VEGFR 抑制剂

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍和1000倍以上。了解更多

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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AZD1480

Catalog No. A10110
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JAK 抑制剂

AZD1480是一种新型有效的小型JAK2抑制剂，IC50为0.26 nM。了解更多

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- Simona Moravcova, .et al. The Circadian Rhythms of STAT3 in the Rat Pineal Gland and Its Involvement in Arylalkylamine-N-Acetyltransferase Regulation, Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476

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